牛蒡子苷自微乳在体肠吸收分析方法学研究  

Analytical methodology on in situ rat intestine absorption of arctiin SMEDDS

作　　者：赵德华[1] 卢来春[2] 管海燕[2] 张卿[2] 尚京川[1] 

机构地区：[1]重庆医科大学药学院药物分析教研室,重庆400016 [2]第三军医大学大坪医院野战外科研究所药剂科,重庆400042

出　　处：《第三军医大学学报》2013年第24期2681-2685,共5页Journal of Third Military Medical University

基　　金：重庆市卫生局中医药科技项目(2012-2-25);科技型中小企业技术创新基金(HC26215113529)~~

摘　　要：目的建立HPLC法测定牛蒡子苷自微乳中牛蒡子苷含量并考察牛蒡子苷自微乳在大鼠小肠吸收情况。方法采用自微乳化释药系统（SMEDDS）技术制备牛蒡子苷自微乳，并运用大鼠在体灌流的方法建立牛蒡子苷大鼠肠吸收模型，以流动相乙腈-水（35：65），流速1mL／min，检测波长280nm为色谱条件，测定自微乳中牛蒡子苷含量及肠循环液中牛蒡子苷、苷元含量，并考察药物的吸收。结果牛蒡子苷含量测定方法在2—200μg／mL浓度范围内，苷元含量测定方法在1～100ng／mL浓度范围内，均具有良好线性，回收率均在95％～105％范围内，日内及日间RSD均小于5％。测得牛蒡子苷自微乳载药量为（40．090±0．001）mg／g；在体肠吸收结果表明在10～50μg／mL范围内，药物单位时间吸收百分率小于25％；牛蒡子苷自微乳在小肠有一定的吸收，但在30min后开始水解为牛蒡子苷元。结论所建HPLC法专属性强，准确度及精密度能够满足牛蒡子苷自微乳以及在体肠吸收液中牛蒡子苷、苷元含量的测定。Object ve To establish an HPLC method for determination of arctiin in self-microemulsify- ing drug delivery system （SMEDDS） and studying its absorption in rat intestines. Methods An in situ recirculation model was established to study the absorption of arctiin SMEDDS in rat intestines. The contents of arctiin and arctigenin and drug absorption were determined by HPLC, with mobile phase of acetonitrile-water （35： 65）, flow rate 1 mL/min, and detection wavelength 248 nm. Results The method showed good linearity in arctiin concentration range of 2 - 200 μg/mL and arctigenin concentration range of 1 - 100 μg/mL, with recovery rate 95% to 105% and inter-day and intra-day RSD less than 5%. The content of arctiin in microe- mulsion was （40.090 ±0.001 ） mg/g. In the concentration range from 10 to 50 μg/mL, arctiin absorption rate was less than 25%. The arctiin SMEDDS had some absorption in rat intestines but started to hydrolyze and pro- duce arctigenin after 30 min. Conclusion The HPLC method with good specificity, accuracy and precision is qualified for determination of arctiin and arctigenin from SMEDDS and intestinal fluids.

关 键 词：HPLC 牛蒡子苷自微乳 在体肠吸收 含量测定 

分 类 号：R282.71[医药卫生—中药学] R944.9[医药卫生—中医学]